400-998-5282
专注多肽 服务科研
400-998-5282
专注多肽 服务科研
Peptide YY (PYY) 是一种肠道激素，可调节食欲和抑制胰腺分泌。Peptide YY (PYY) 可以通过神经肽 Y 受体 (Neuropeptide Y receptors) 介导其作用。
编号：132375
CAS号：118997-30-1
单字母：H2N-YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY-CONH2
| 参考文献（References）: | Gerald, C., Walker, M.W., Criscione, L., et al. A receptor subtype involved in neuropeptide-Y-induced food intake. Nature 382(6587), 168-171 (1996). Mullins, D.E., Guzzi, M., Xia, L., et al. Pharmacological characterization of the cloned neuropeptide Y y6 receptor. Eur. J. Pharmacol. 395(2), 87-93 (2000). Holzer, P., Reichmann, F., and Farzi, A. Neuropeptide Y, peptide YY and pancreatic polypeptide in the gut-brain axis. Neuropeptides 46(6), 261-274 (2012). K. Tatemoto et al., Nature, 285, 417 (1980) K. Tatemoto, PNAS, 79, 2514 (1982) |
Peptide YY (PYY) 是一种肠道激素，可调节食欲和抑制胰腺分泌。Peptide YY (PYY) 可以通过神经肽 Y 受体 (Neuropeptide Y receptors) 介导其作用。
Peptide YY (PYY) is a gut hormone that regulates appetite and inhibits pancreatic secretion. Peptide YY (PYY) can mediate its effects through the Neuropeptide Y receptors.
肽YY（PYY）是一种36个氨基酸的肽，是神经肽Y受体Y1、Y2、Y5和Y6的厌食肠道激素激动剂，EC50值分别为0.7、0.58、1和0.8 nM，用于抑制福司柯林诱导的cAMP积累。PYY在体内被切割成PYY（3-36）。PYY的释放发生在餐后，与肠道内分泌L细胞的热量摄入成比例，表明这可能是一种饱腹感信号。在人类中，PYY抑制了瘦和肥胖受试者的食物摄入和胃肠道转运。
Peptide YY (PYY) is a 36-amino acid peptide and anorectic gut hormone agonist for the neuropeptide Y receptors Y1, Y2, Y5, and Y6 with EC50 values of 0.7, 0.58, 1, and 0.8 nM, respectively, for supression of forskolin-induced cAMP accumulation. PYY is cleaved in vivo to PYY (3-36) . Release of PYY occurs postprandially in proportion to calorie intake from intestinal enteroendocrine L cells, indicating it may be a satiety signal. In humans, PYY inhibits food intake and gastrointestinal transit in both lean and obese subjects.
肽主要存在于胃肠道中，据信与喂养行为有关。
Peptide mainly found in gastrointestinal tract that is believed to involve the feeding behavior.
多肽YY(Peptide YY)的定义
多肽YY（PYY）是胃肠道合成和分泌的一种重要肠道激素。
Peptide YY (PYY) is an important gut hormone synthesized and secreted by the gastrointestinal tract.
多肽YY(Peptide YY)的相关肽
PYY是一种直链多肽。PYY与神经肽Y（NPY）和胰多肽（PP）【1】具有结构同源性，共同形成神经肽Y肽家族，也称为胰多肽折叠肽家族。
PYY is a straight chain polypeptide. PYY shares structural homology with neuropeptide Y (NPY) and pancreatic polypeptide (PP) 【1】, and together form the Neuropeptide Y Family of Peptides, which is also called the Pancreatic Polypeptide-Fold Family of Peptides.
PP肽家族包括PYY和NPY，它们是根据其化学结构（具有羧基末端酪氨酸酰胺）【2】发现的。PP、PYY和NPY的长度均为36个氨基酸，尽管结构相似；它们存在于胃肠道和神经系统的不同部位，具有不同的生物学作用。PP在肠道和胰腺的内分泌细胞中表达，PYY位于回肠和结肠的肠内分泌细胞以及肠神经系统的神经中，NPY存在于中枢和外周神经系统中。这种广泛的分布表明，这些肽调节许多不同的生理过程。
The PP family of peptides includes PYY and NPY, which were discovered based upon their chemical structure (possessing a carboxyl-terminal tyrosine amide) 【2】. PP, PYY, and NPY are all 36 amino acids in length and despite structural similarities; they are found in different locations throughout the gastrointestinal tract and nervous system and possess different biological actions. PP is expressed in endocrine cells of the gut and pancreas, PYY is located in enteroendocrine cells of the ileum and colon and nerves of the enteric nervous system, and NPY is found in the central and peripheral nervous system. This wide distribution suggests that these peptides regulate many different physiological processes.
多肽YY(Peptide YY)的结构特征
人PYY由36个氨基酸残基的线性链组成，完整的氨基酸序列为：Tyr-Pro-Ile-Lys-Pro-Glu-Ala-Pro-Gly-Glu-Asp-Ala-Ser-Pro-Glu-Glu-Leu-Asn-Arg-Tyr-Tyr-Ala-Ser-Leu-Arg-His-Tyr-Leu-Asn-Leu-Val-Thr-Arg-Gln-Arg-Tyr-NH2。猪和人PYY的结构差异在3位（Ala/Ile置换）和18位（Ser/Asn）。发现使用固相合成技术制备的合成人PYY在结构上与天然肽相同【3】。
Human PYY consists of a linear chain of 36 amino acid residues and the complete amino acid sequence is: Tyr-Pro-Ile-Lys-Pro-Glu-Ala-Pro-Gly-Glu-Asp-Ala-Ser-Pro-Glu-Glu-Leu-Asn-Arg-Tyr-Tyr-Ala-Ser-Leu-Arg-His-Tyr-Leu-Asn-Leu-Val-Thr-Arg-Gln-Arg-Tyr-NH2. The differences between the structures of porcine and human PYY are at positions 3 (Ala/Ile replacement) and 18 (Ser/Asn). Synthetic human PYY prepared using a solid-phase synthetic technique was found to be structurally identical to the natural peptide【3】.
多肽YY(Peptide YY)的作用方式
PYY与胰高血糖素样肽1共分泌。PYY由肠道L细胞产生，在胃肠道的远端段发现了最高的组织浓度，尽管它存在于整个肠道中。PYY的释放受到管腔内营养物质的刺激，包括葡萄糖、胆汁盐、脂质、短链脂肪酸和氨基酸。胆囊收缩素（CCK）、血管活性肠多肽（VIP）、胃泌素和GLP-1等调节肽调节PYY的释放。近端胃肠道也可能通过迷走神经纤维参与PYY释放的调节。释放后，二肽基肽酶IV（DPP-IV；CD 26）切割N端酪氨酸脯氨酸残基，形成PYY（3-36）。PYY（1-36）占循环PYY的约60%，PYY（3-36）占40%。PYY通过人类Y受体亚型Y1、Y2、Y4和Y5起作用。PYY（1-36）对所有四种受体显示出高亲和力，而PYY（3-36）是一种特异性Y2激动剂。PYY抑制许多胃肠道功能，包括胃酸分泌、胃排空、小肠和结肠氯化物分泌、口腔到盲肠的转运时间、胰腺外分泌和胰腺胰岛素分泌。PYY还可以促进餐后自然排尿，提高收缩压和舒张压【4，5】。
PYY is co-secreted with glucagon-like peptide 1. Produced by the intestinal L-cells, the highest tissue concentrations of PYY are found in distal segments of the gastrointestinal tract, although it is present throughout the gut. PYY release is stimulated by intraluminal nutrients, including glucose, bile salts, lipids, short-chain fatty acids and amino acids. Regulatory peptides such as cholecystokinin (CCK), vasoactive intestinal polypeptide (VIP), gastrin and GLP-1 modulate PYY release. The proximal GI tract may also participate in the regulation of PYY release through vagal fibers. After release, dipeptidyl peptidase IV (DPP-IV; CD 26) cleaves the N-terminal tyrosine-proline residues forming PYY (3-36). PYY (1-36) represents about 60% and PYY (3-36) 40% of circulating PYY. PYY acts through Y-receptor subtypes: Y1, Y2, Y4 and Y5 in humans. PYY (1-36) shows high affinity to all four receptors while PYY (3-36) is a specific Y2 agonist. PYY inhibits many GI functions, including gastric acid secretion, gastric emptying, small bowel and colonic chloride secretion, mouth to cecum transit time, pancreatic exocrine secretion and pancreatic insulin secretion. PYY also promotes postprandial naturesis and elevates systolic and diastolic blood pressure【4，5】.
多肽YY(Peptide YY)的功能
PYY作为肠上皮生长因子：PYY是一种丰富的远端肠道激素，可能在肠上皮增殖中发挥重要作用。肠上皮细胞表达PYY的特异性受体，PYY在体内和体外诱导肠细胞增殖，Y1受体亚型与促有丝分裂信号通路偶联。除了对肠道粘膜维持的拟议生理作用外，PYY增殖作用可能被假设为促进刺激生长的病理生理后果【6】。
PYY as a growth factor for intestinal epithelium: PYY is an abundant distal gut hormone that may play a significant role in intestinal epithelial proliferation. Gut epithelial cells express specific receptors for PYY, PYY induces proliferation in intestinal cells in vivo and in vitro, and the Y1 receptor subtype couples to mitogenic signaling pathways. In addition to proposed physiologic effects on gut mucosal maintenance, PYY proliferative effects may be hypothesized to contribute to pathophysiologic consequences of stimulated growth【6】.
PYY、食欲和食物摄入：随着食物摄入，PYY被释放到循环中。PYY浓度与膳食能量含量成正比，峰值血浆水平出现在餐后1小时后。PYY3-36是肠粘膜内分泌细胞和循环中PYY的主要形式。PYY3-36的外周给药在啮齿动物和人类中抑制食物摄入数小时。PYY3-36-与Y2受体的结合导致NPY神经元的抑制，并可能对促阿片黑皮质素神经元产生相互刺激。因此，PYY3-36似乎通过对下丘脑回路提供强大的反馈来控制食物摄入。PYY3-36对食物摄入的影响已在生理浓度下得到证实，因此，PYY3-36s可能在日常食物摄入调节中很重要【7】。
PYY, appetite and food intake: Following food intake PYY is released into the circulation. PYY concentrations are proportional to meal energy content and peak plasma levels appear postprandially after 1 hr. PYY3-36 is a major form of PYY in both the gut mucosal endocrine cells and the circulation. Peripheral administration of PYY3-36 inhibits food intake for several hours in both rodents and man. The binding of PYY3-36 to the Y2 receptor leads to an inhibition of the NPY neurones and a possible reciprocal stimulation of the pro-opiomelanocortin neurones. Thus, PYY3-36 appears to control food intake by providing a powerful feedback on the hypothalamic circuits. The effect on food intake has been demonstrated at physiological concentrations and, therefore, PYY3-36 may be important in the everyday regulation of food intake【7】.
PYY对胃酸分泌的中枢和外周调节：餐后从回肠和结肠释放的PYY通过中枢和外周机制显示出对胃酸分泌头相和胃相的强烈抑制作用。为了调节迷走神经对胃功能的调节，循环的PYY通过最后区和孤束核进入大脑，在那里它通过PYY偏好Y1样受体发挥刺激作用，并通过Y2受体发挥抑制作用。在胃黏膜中，PYY与肠嗜铬样细胞中的Y1受体结合，通过百日咳毒素敏感途径抑制胃泌素刺激的组胺释放和钙信号传导【8】。
Central and peripheral regulation of gastric acid secretion by PYY: PYY released postprandially from the ileum and colon displays a potent inhibition of cephalic and gastric phases of gastric acid secretion through both central and peripheral mechanisms. To modulate vagal regulation of gastric functions, circulating PYY enters the brain through the area postrema and the nucleus of the solitary tract, where it exerts a stimulatory action through PYY-preferring Y1-like receptors, and an inhibitory action through Y2 receptors. In the gastric mucosa, PYY binds to Y1 receptors in the enterochromaffin-like cells to inhibit gastrin-stimulated histamine release and calcium signaling via a pertussis toxin-sensitive pathway【8】.
多肽YY(Peptide YY)的相关文献
1. Tatemoto K, Carlquist M, Mutt V (1982). Neuropeptide Y--a novel brain peptide with structural similarities to peptide YY and pancreatic polypeptide. Nature, 296(5858):659-660.
2. Tatemoto K (1982). Neuropeptide Y: Complete amino acid sequence of the brain peptide. PNAS., 79(18):5485-5489.
3. Tatemoto K, Nakano I, Makk G, Angwin P, Mann M, Schilling J, Go VL (1988). Isolation and primary structure of human peptide YY. Biochem Biophys Res Commun., 157(2):713-717.
4. Ballantyne GH (2006). Peptide YY (1-36) and peptide YY(3-36): Part I. Distribution, release and actions. Obes Surg., 16(5):651-658.
5. Batterham RL, Bloom SR (2003). The gut hormone peptide YY regulates appetite. Ann N Y Acad Sci., 994:162-168.
6. Mannon PJ (2002). Peptide YY as a growth factor for intestinal epithelium. Peptides, 23(2):383-388.
7. Ie Roux CW, Bloom SR (2005). Peptide YY, appetite and food intake. Proc Nutr Soc., 64(2):213-216.
8. Yang H (2002). Central and peripheral regulation of gastric acid secretion by peptide YY. Peptides, 23(2):349-358.
| DOI | 名称 | |
|---|---|---|
| 10.1073/pnas.79.8.2514 | Isolation and characterization of peptide YY (PYY), a candidate gut hormone that inhibits pancreatic exocrine secretion | 下载 |
| 10.1111/j.1749-6632.2003.tb03176.x | The gut hormone peptide YY regulates appetite | 下载 |
| 10.1111/1440-1681.12398 | Role of Peptide YY in blood vessel function and atherosclerosis in a rabbit model | 下载 |
多肽H2N-Tyr-Pro-Ile-Lys-Pro-Glu-Ala-Pro-Gly-Glu-Asp-Ala-Ser-Pro-Glu-Glu-Leu-Asn-Arg-Tyr-Tyr-Ala-Ser-Leu-Arg-His-Tyr-Leu-Asn-Leu-Val-Thr-Arg-Gln-Arg-Tyr-NH2的合成步骤：
1、合成MBHA树脂：取若干克的MBHA树脂（如初始取代度为0.5mmol/g）和1倍树脂摩尔量的Fmoc-Linker-OH加入到反应器中，加入DMF，搅拌使氨基酸完全溶解。再加入树脂2倍量的DIEPA，搅拌混合均匀。再加入树脂0.95倍量的HBTU，搅拌混合均匀。反应3-4小时后，用DMF洗涤3次。用2倍树脂体积的10%乙酸酐/DMF 进行封端30分钟。然后再用DMF洗涤3次，甲醇洗涤2次，DCM洗涤2次，再用甲醇洗涤2次。真空干燥12小时以上，得到干燥的树脂{Fmoc-Linker-MHBA Resin}，测定取代度。这里测得取代度为 0.3mmol/g。结构如下图：
2、脱Fmoc：取2.42g的上述树脂，用DCM或DMF溶胀20分钟。用DMF洗涤2遍。加3倍树脂体积的20%Pip/DMF溶液，鼓氮气30分钟，然后2倍树脂体积的DMF 洗涤5次。得到 H2N-Linker-MBHA Resin 。（此步骤脱除Fmoc基团，茚三酮检测为蓝色，Pip为哌啶）。结构图如下：
3、缩合：取2.18mmol Fmoc-Tyr(tBu)-OH 氨基酸，加入到上述树脂里，加适当DMF溶解氨基酸，再依次加入4.36mmol DIPEA，2.07mmol HBTU。反应30分钟后，取小样洗涤，茚三酮检测为无色。用2倍树脂体积的DMF 洗涤3次树脂。（洗涤树脂，去掉残留溶剂，为下一步反应做准备）。得到Fmoc-Tyr(tBu)-Linker-MBHA Resin。氨基酸：DIPEA：HBTU：树脂=3：6：2.85：1（摩尔比）。结构图如下：
4、依次循环步骤二、步骤三，依次得到
H2N-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Ile-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Ile-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Pro-Ile-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
H2N-Pro-Ile-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
Fmoc-Tyr(tBu)-Pro-Ile-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin
以上中间结构，均可在专肽生物多肽计算器-多肽结构计算器中，一键画出。
最后再经过步骤二得到 H2N-Tyr(tBu)-Pro-Ile-Lys(Boc)-Pro-Glu(OtBu)-Ala-Pro-Gly-Glu(OtBu)-Asp(OtBu)-Ala-Ser(tBu)-Pro-Glu(OtBu)-Glu(OtBu)-Leu-Asn(Trt)-Arg(Pbf)-Tyr(tBu)-Tyr(tBu)-Ala-Ser(tBu)-Leu-Arg(Pbf)-His(Trt)-Tyr(tBu)-Leu-Asn(Trt)-Leu-Val-Thr(tBu)-Arg(Pbf)-Gln(Trt)-Arg(Pbf)-Tyr(tBu)-Linker-MBHA Resin，结构如下：
5、切割：6倍树脂体积的切割液（或每1g树脂加8ml左右的切割液），摇床摇晃 2小时，过滤掉树脂，用冰无水乙醚沉淀滤液，并用冰无水乙醚洗涤沉淀物3次，最后将沉淀物放真空干燥釜中，常温干燥24小试，得到粗品H2N-Tyr-Pro-Ile-Lys-Pro-Glu-Ala-Pro-Gly-Glu-Asp-Ala-Ser-Pro-Glu-Glu-Leu-Asn-Arg-Tyr-Tyr-Ala-Ser-Leu-Arg-His-Tyr-Leu-Asn-Leu-Val-Thr-Arg-Gln-Arg-Tyr-NH2。结构图见产品结构图。
切割液选择：1）TFA：H2O=95%：5%
2）TFA：H2O：TIS=95%：2.5%：2.5%
3）三氟乙酸：茴香硫醚：1，2-乙二硫醇：苯酚：水=87.5%：5%：2.5%：2.5%：2.5%
（前两种适合没有容易氧化的氨基酸，例如Trp、Cys、Met。第三种适合几乎所有的序列。）
6、纯化冻干：使用液相色谱纯化，收集目标峰液体，进行冻干，获得蓬松的粉末状固体多肽。不过这时要取小样复测下纯度 是否目标纯度。
7、最后总结：
杭州专肽生物技术有限公司（ALLPEPTIDE https://www.allpeptide.com）主营定制多肽合成业务，提供各类长肽，短肽，环肽，提供各类修饰肽，如：荧光标记修饰（CY3、CY5、CY5.5、CY7、FAM、FITC、Rhodamine B、TAMRA等），功能基团修饰肽（叠氮、炔基、DBCO、DOTA、NOTA等），同位素标记肽（N15、C13），订书肽（Stapled Peptide）,脂肪酸修饰肽（Pal、Myr、Ste），磷酸化修饰肽（P-Ser、P-Thr、P-Tyr），环肽（酰胺键环肽、一对或者多对二硫键环），生物素标记肽，PEG修饰肽，甲基化修饰肽等。
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